DE4227806A1 - Topical compsn. for lightening skin or skin spots - contg. flavonoid, reducing agent for dopa-quinone and opt. sun protectant, suppressant for tyrosinase activity and tocopherol deriv. - Google Patents

Topical compsn. for lightening skin or skin spots - contg. flavonoid, reducing agent for dopa-quinone and opt. sun protectant, suppressant for tyrosinase activity and tocopherol deriv.

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Publication number
DE4227806A1
DE4227806A1 DE4227806A DE4227806A DE4227806A1 DE 4227806 A1 DE4227806 A1 DE 4227806A1 DE 4227806 A DE4227806 A DE 4227806A DE 4227806 A DE4227806 A DE 4227806A DE 4227806 A1 DE4227806 A1 DE 4227806A1
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skin
composition according
flavonoid
deriv
acid
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German (de)
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Nira Hadas
Meir Stern
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Fischer Pharmaceuticals Ltd
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Fischer Pharmaceuticals Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/046—Aerosols; Foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/29—Titanium; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35—Ketones, e.g. benzophenone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/678—Tocopherol, i.e. vitamin E
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782—Enzyme inhibitors; Enzyme antagonists

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Inorganic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

A compsn. for topical use, for lightening the skin and skin spots, as a soln., lotion, gel, spray or cream, contains a combination of (a) an active amt. of a flavonoid and (b) an active amt. of DOPA-quinone reducing agent, opt with (c) a sun protectant, (d) an agent for suppressing tyrosinase activity and/or (e) a tocopheryl deriv.. (a) The component is pref. 0.1-30 wt.% of a plant extract or purified prepn. from Achillea millofolium, Calendula, sage, witchhazel and mulberry, or of licorice (Glycyrrhiza glubra). (b) The component is 0.1-5 wt.% of ascorbic acid (pref.), ascorbyl palmitate or stearate, Mg ascorbyl phosphate or other physiologically acceptable deriv. of ascorbic acid. (c) The component is 0.1-10% of an agent giving protection against UVA, UVB, IR and/or visible light, e.g. octylmethoxy-cinomate, butylmethoxydibenzoylmethane and TiO2. The compsn. also contains a tocopheryl deriv. and 0.1-5% of kojic acid. A cosmetic skin lightener for topoical use, contg. ascorbic acid or a deriv. and a flavonoid, and opt. with other components, diluents, cream bases and/or gel-formers, is claimed. ADVANTAGE - The skin is lightened, and formation of new brown spots on the skin is largely prevented. The components have a synerigistic effec

Description

Die Erfindung betrifft neue kosmetische Zusammensetzungen zur topischen Anwendung. Bei diesen Zusammensetzungen handelt es sich um Bleichmittel, die in beliebiger herkömmlicher Form zur topischen Anwendung, wie Cremes, Gele, Lotionen, Sprühmittel und dgl., vorliegen können.The invention relates to novel cosmetic compositions for topical use. In these compositions are bleaches that are in any conventional form for topical application, such as creams, Gels, lotions, sprays and the like., May be present.

Die Bleichmittel führen beim Anwender zu einer Hautaufhel­ lung und verhindern weitgehend die Bildung von neuen dunklen Flecken auf der Haut des Anwenders.The bleaches cause the user to a Hautaufhel and largely prevent the formation of new dark ones Stains on the skin of the user.

Die Pigmentbildung in der Haut erfolgt in den Melanozyten. Die Melanozyten bilden Melanosome, membrangebundene Organel­ len im Zytoplasma der Melanozyten, die sodann auf benach­ barte Keratinozyten übertragen werden. Melanin, das inner­ halb der Melanosomen gebildet wird, ist für die Grundfarbe der menschlichen Haut verantwortlich. Beim biosynthetischen Melanin-Stoffwechselweg spielt Tyrosinase, ein kupferhalti­ ges Enzym, eine wichtige Rolle bezüglich des Ausmaßes der Pigmentbildung. Eine Hautfärbung tritt nur dann auf, wenn Melanosomen mit einem Gehalt an Melanin auf die Keratinozyten übertragen werden.The pigmentation in the skin takes place in the melanocytes. The melanocytes form melanosomes, membrane-bound organelles in the cytoplasm of the melanocytes, which then keratinocytes are transmitted. Melanin, the inner Half of the melanosomes is formed for the primary color responsible for the human skin. When biosynthetic Melanin metabolic pathway plays tyrosinase, a copper content enzyme, an important role in the extent of the  Pigment formation. Skin coloration only occurs when Melanosomes containing melanin on the Keratinocytes are transmitted.

Verschiedene Faktoren, darunter die genetische Steuerung und Umweltfaktoren, wie UV-Strahlung und Hormone, steuern die Melanogenese. Eine abnormale Reaktion der Melanozyten auf diese Faktoren kann zu einer verstärkten Anreicherung von Melanin in der Haut in Form von braunen Flecken führen.Various factors, including genetic control and Environmental factors, such as UV radiation and hormones, control the Melanogenesis. An abnormal response of the melanocytes to These factors can lead to increased accumulation of Melanin in the skin in the form of brown spots lead.

Die Erfindung betrifft neue kosmetische Zusammensetzungen zur topischen Anwendung auf die Haut, die zu einer Aufhel­ lung der Haut führen und die Bildung von braunen Flecken weitgehend verhindern.The invention relates to novel cosmetic compositions for topical application to the skin, resulting in an Skin development and the formation of brown spots largely prevent.

Die erfindungsgemäßen Zusammensetzungen enthalten eine Kom­ bination aus Flavonoiden, die zu einer Beseitigung oder zu­ mindest zu einer weitgehenden Mengenreduzierung der Pig­ mente, die sich aufgrund von UV-Strahlung in der Haut bil­ den, führen, und Ascorbinsäure oder einem geeigneten Derivat davon. Ascorbinsäure (oder ihre physiologisch verträglichen Derivate) führt zur Reduktion von DOPA-Chinon zu DOPA und auch zur Umwandlung von gefärbtem, oxidiertem Melanin zu dessen farbloser, reduzierter Form. Vorteilhafterweise wer­ den Flavonoide, die sich aus Pflanzenextrakten ableiten oder Pflanzenextrakte als solche, die eine geeignete Konzentra­ tion an derartigen Flavonoiden enthalten, verwendet. Es kön­ nen auch synthetische Flavonoide eingesetzt werden. Die er­ findungsgemäßen Zusammensetzungen eignen sich auch zur Ver­ ringerung der Melaninbildung in den frühen Bildungsstadien oder zur Verhinderung der Bildung von neuen Flecken. Die neuartigen erfindungsgemäßen Bleichmittel üben eine ausge­ prägte weißmachende und aufhellende Wirkung auf braune Haut­ flecken aus. The compositions of the invention contain a com from flavonoids leading to elimination or to at least to a substantial reduction in the amount of pig which forms in the skin due to UV radiation lead, and ascorbic acid or a suitable derivative from that. Ascorbic acid (or its physiologically tolerated Derivatives) leads to the reduction of DOPA-quinone to DOPA and also for the conversion of colored, oxidized melanin its colorless, reduced form. Advantageously who the flavonoids derived from plant extracts or Plant extracts as such, which are suitable concentra tion of such flavonoids used. It can Synthetic flavonoids can also be used. He compositions according to the invention are also suitable for Ver Reduction of melanin formation in the early stages of education or to prevent the formation of new stains. The novel bleach according to the invention exert an out coined whitening and lightening effect on brown skin blot out.  

Bevorzugte Pflanzenextrakte für die erfindungsgemäße Verwen­ dung sind solche die aus Achillea millefolium, Calendula, Salbei, Zaubernuß und Maulbeere erhalten worden sind.Preferred plant extracts for the use according to the invention These are Achillea millefolium, Calendula, Sage, witch hazel and mulberry have been obtained.

Die erfindungsgemäßen Präparate enthalten einen geeigneten Träger sowie einen oder mehrere zusätzliche Bestandteile, die unter Tocopherolderivaten, Kojisäure, chemischen und physikalischen Sonnenschutzmitteln im UVA-, UVB- und sicht­ baren Bereich und Mineralstoffen, wie Titandioxid, ausgewählt sind. Zu geeigneten Sonnenschutzmitteln gehören handelsübliche Produkte, wie Octylmethoxycinnamat, Butylmethoxydibenzoylmethan und dgl. Eine Vielzahl von Formulierungen kann eingesetzt werden. Nachstehend finden sich typische Beispiele für derartige Formulierungen.The preparations according to the invention contain a suitable Carrier and one or more additional components, Among the tocopherol derivatives, kojic acid, and chemical physical sunscreens in the UVA, UVB and view range and minerals, such as titanium dioxide, are selected. To include suitable sunscreen commercially available products, such as octyl methoxycinnamate, Butylmethoxydibenzoylmethane and the like. A variety of Formulations can be used. Find below typical examples of such formulations.

Im allgemeinen enthalten die erfindungsgemäßen Formulierun­ gen ab etwa 0,1 Gew.-% eines Extrakts von einem oder mehreren der folgenden Pflanzen: Achillea millefolium, Calendula, Salbei, Zaubernuß und Maulbeere. Es können auch andere Pflanzenextrakte mit einem Gehalt an merklichen Mengen an Flavonoiden verwendet werden. Die Formulierungen enthalten im allgemeinen etwa 0,1 bis etwa 30 Gew.-% an derartigen Pflanzenextrakten oder eine entsprechende Menge an gereinigten Flavonoiden. Beim zweiten Bestandteil handelt es sich um ein physiologisch verträgliches Derivat von Ascorbinsäure, wie Ascorbylpalmitat, Ascorbylstearat, Magnesiumascorbylphosphat und dgl. Der zweite Bestandteil ist in einer Menge von etwa 0,1 bis etwa 5 Gew.-% in der Zusammensetzung enthalten.In general, the formulations according to the invention contain from about 0.1% by weight of an extract of one or more several of the following plants: Achillea millefolium, Calendula, sage, witch hazel and mulberry. It can too other plant extracts containing appreciable Amounts of flavonoids are used. The formulations generally contain from about 0.1 to about 30 weight percent such plant extracts or an appropriate amount on purified flavonoids. The second component is it is a physiologically acceptable derivative of Ascorbic acid, such as ascorbyl palmitate, ascorbyl stearate, Magnesium ascorbyl phosphate and the like. The second ingredient is in an amount of about 0.1 to about 5 wt .-% in the Composition included.

Lakritzenextrakt in einer Menge von 0,01 bis etwa 5 Gew.-% stellt einen bevorzugten Bestandteil dar.Licorice extract in an amount of 0.01 to about 5% by weight represents a preferred component.

Die Formulierungen enthalten vorteilhafterweise auch einen als Sonnenschutzmittel wirkenden Bestandteil, der beispiels­ weise gegen UVA-Licht, UVB-Licht und sichtbares Licht schützt, wie Octylmethoxycinnamat, Butylmethoxydibenzoylme­ than und dgl. Eine weitere Substanz mit ähnlicher Wirkung ist TiO2. Im allgemeinen machen diese Bestandteile etwa 2 bis etwa 10 Gew.-% der Formulierung aus. Ein weiterer fakul­ tativer, vorteilhafter Bestandteil ist ein geeignetes Toco­ pherylderivat, wie Tocopheryllinoleat. Verbindungen dieses Typs sind gegebenenfalls in einer Menge von 0,1 bis etwa 5 Gew.-% der Formulierung enthalten.The formulations advantageously also contain a sunscreen-acting ingredient which protects, for example, against UVA light, UVB light and visible light, such as octyl methoxycinnamate, butyl methoxydibenzoylmethane and the like. Another substance having a similar effect is TiO 2 . In general, these ingredients make up about 2 to about 10% by weight of the formulation. Another fakul tative, beneficial ingredient is a suitable Toco pherylderivat such as tocopheryl linoleate. Compounds of this type are optionally included in an amount of from 0.1% to about 5% by weight of the formulation.

Ein weiterer fakultativer, vorteilhafter Bestandteil, der vermutlich aufgrund der Kupfer-Chelatbildung zur Unter­ drückung der Tyrosinase-Aktivität geeignet ist, ist Koji­ säure. Dieser Bestandteil wird in einer Konzentration von etwa 0,1 bis 5 Gew.-% der Formulierung verwendet.Another optional, beneficial ingredient that probably due to copper chelation to sub Pressing the tyrosinase activity is suitable Koji acid. This ingredient is in a concentration of about 0.1 to 5 wt .-% of the formulation used.

Nachstehend wird die Erfindung anhand von Beispielen, die die Herstellung von Cremes, Lotionen, Sprühmitteln und Gelen beschreiben, näher erläutert.Hereinafter, the invention by way of examples, the the preparation of creams, lotions, sprays and gels describe, explained in more detail.

Beispiel 1: CremeExample 1: Cream Extrakt von Achillea millefolium|20%Extract of Achillea millefolium | 20% MagnesiumascorbylpalmitatMagnesiumascorbylpalmitat 5%5% Cremegrundlage, adCream base, ad 100100

Beispiel 2: CremeExample 2: cream Maulbeerenextrakt|25%Mulberry extract | 25% Ascorbinsäureascorbic acid 0,1%0.1% Cremegrundlage, adCream base, ad 100100

Beispiel 3: CremeExample 3: Cream Extrakt von Achillea millefolium|15%Extract of Achillea millefolium | 15% Ascorbylstearatascorbyl 5%5% TiO₂TiO₂ 10%10% Cremegrundlage, adCream base, ad 100100

Beispiel 4: LotionExample 4: Lotion Extrakt von Achillea millefolium|10%Extract of Achillea millefolium | 10% Ascorbylpalmitatascorbyl 0,5%0.5% Octylmethoxycinnamatoctyl 7,5%7.5% Butylmethoxydibenzoylmethanbutylmethoxydibenzoylmethane 0,5%0.5% TiO₂TiO₂ 10%10% Kojisäurekojic acid 3%3% Lotionsgrundlage, adLotion base, ad 100100

Beispiel 5: LotionExample 5: Lotion Extrakt von Achillea millefolium|5%Extract of Achillea millefolium | 5% Ascorbylpalmitatascorbyl 0,5%0.5% Benzophenonbenzophenone 5%5% TiO₂TiO₂ 10%10% Tocopheryllinoleattocopheryl 1%1% Lotionsgrundlage, adLotion base, ad 100100

Beispiel 6: LotionExample 6: Lotion Kojisäure|2%Kojic acid | 2% TiO₂TiO₂ 5%5% Lotionsgrundlage, adLotion base, ad 100100

Beispiel 7: GelExample 7: Gel Kojisäure|0,1%Kojic acid | 0.1% UVA- & UVB-SonnenschutzmittelUVA & UVB sunscreen 5%5% Gelgrundlage, adGel base, ad 100100

Beispiel 8: LotionExample 8: Lotion Ascorbylpalmitat|0,2%Ascorbyl | 0.2% Tocopheryllinoleattocopheryl 3%3% Kojisäurekojic acid 0,5%0.5% Lotionsgrundlage, adLotion base, ad 100100

Beispiel 9: CremeExample 9: Cream Bestandteileingredients %% Ascorbylpalmitatascorbyl 44 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 11 Tocopheryllinoleattocopheryl 0,10.1 Octylmethoxycinnamatoctyl 22 Butylmethoxydibenzoylmethanbutylmethoxydibenzoylmethane 0,750.75 TiO₂TiO₂ 11 Kojisäurekojic acid 0,10.1 Panthenolpanthenol 11 Kamillenextraktchamomile extract 0,10.1 IPMIPM 22 BHTBHT 0,040.04 Konservierungsmittelpreservative 0,50.5 Stearinsäurestearic acid 44 Na₂EDTANa₂EDTA 0,10.1 DEA-CetylphosphatDEA cetyl phosphate 3,53.5 Cetylalkoholcetyl alcohol 22 Glycerinstearatglyceryl stearate 44 destilliertes Wasser, addistilled water, ad 100100

Beispiel 10: CremeExample 10: Cream Bestandteileingredients %% Ascorbylpalmitatascorbyl 0,10.1 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 3030 Tocopheryllinoleattocopheryl 55 Octylmethoxycinnamatoctyl 77 Butylmethoxydibenzoylmethanbutylmethoxydibenzoylmethane 33 TiO₂TiO₂ 1010 Kojisäurekojic acid 55 Panthenolpanthenol 11 Kamillenextraktchamomile extract 0,10.1 IPMIPM 22 BHTBHT 0,040.04 Konservierungsmittelpreservative 0,50.5 Stearinsäurestearic acid 44 Na₂EDTANa₂EDTA 0,10.1 DEA-CetylphosphatDEA cetyl phosphate 3,53.5 Cetylalkoholcetyl alcohol 22 Glycerinstearatglyceryl stearate 44 destilliertes Wasser, addistilled water, ad 100100

Beispiel 11: LotionExample 11: Lotion Bestandteileingredients %% Ascorbylpalmitatascorbyl 0,10.1 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 3030 Tocopheryllinoleattocopheryl 55 Octylmethoxycinnamatoctyl 77 Butylmethoxydibenzoylmethanbutylmethoxydibenzoylmethane 33 TiO₂TiO₂ 1010 Kojisäurekojic acid 55 Panthenolpanthenol 11 Kamillenextraktchamomile extract 0,10.1 IPMIPM 22 BHTBHT 0,040.04 Konservierungsmittelpreservative 0,50.5 Stearinsäurestearic acid 22 Na₂EDTANa₂EDTA 0,10.1 DEA-CetylphosphatDEA cetyl phosphate 3,53.5 Cetylalkoholcetyl alcohol 0,20.2 Glycerinstearatglyceryl stearate 22 destilliertes Wasser, addistilled water, ad 100100

Beispiel 12: LotionExample 12: Lotion Bestandteileingredients %% Ascorbylpalmitatascorbyl 44 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 11 Tocopheryllinoleattocopheryl 0,10.1 Octylmethoxycinnamatoctyl 22 Butylmethoxydibenzoylmethanbutylmethoxydibenzoylmethane 0,750.75 TiO₂TiO₂ 11 Kojisäurekojic acid 0,10.1 Panthenolpanthenol 11 Kamillenextraktchamomile extract 0,10.1 IPMIPM 22 BHTBHT 0,040.04 Konservierungsmittelpreservative 0,50.5 Stearinsäurestearic acid 22 Na₂EDTANa₂EDTA 0,10.1 DEA-CetylphosphatDEA cetyl phosphate 3,53.5 Glycerinstearatglyceryl stearate 22 destilliertes Wasser, addistilled water, ad 100100

Beispiel 13: GelExample 13: Gel Bestandteileingredients %% Ascorbylpalmitatascorbyl 0,50.5 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 11 Polysorbatpolysorbate 66 CarbopolCarbopol 11 Triethanolamintriethanolamine 4,24.2 Konservierungsmittelpreservative 11 Kojisäurekojic acid 55 TiO₂TiO₂ 11 Tocopheryllinoleattocopheryl 22 Panthenolpanthenol 11 Phenylbenzimidazol-5-sulfonsäurePhenylbenzimidazole-5-sulfonic acid 66 Wasser, adWater, ad 100100

Beispiel 14: GelExample 14: Gel Bestandteileingredients %% Ascorbylpalmitatascorbyl 33 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 2525 Tocopheryllinoleattocopheryl 0,50.5 Polysorbatpolysorbate 66 CarbopolCarbopol 11 Triethanolamintriethanolamine 1,61.6 Konservierungsmittelpreservative 11 Kojisäurekojic acid 0,10.1 Phenylbenzimidazol-5-sulfonsäurePhenylbenzimidazole-5-sulfonic acid 0,10.1 TiO₂TiO₂ 11 Panthenolpanthenol 11 Wasser, adWater, ad 100100

Beispiel 15: FlüssigkeitExample 15: Liquid Bestandteileingredients %% Ascorbylpalmitatascorbyl 33 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 2525 Tocopheryllinoleattocopheryl 0,50.5 Polysorbatpolysorbate 1010 Triethanolamintriethanolamine 0,050.05 Konservierungsmittelpreservative 11 Kojisäurekojic acid 0,10.1 Phenylbenzimidazol-5-sulfonsäurePhenylbenzimidazole-5-sulfonic acid 0,10.1 TiO₂TiO₂ 1010 Panthenolpanthenol 11 Wasser, adWater, ad 100100

Beispiel 16: FlüssigkeitExample 16: Liquid Bestandteileingredients %% Ascorbylpalmitatascorbyl 0,50.5 Achillea millefolium, wasserlöslicher Extrakt (mit einem Gehalt an 3% Flavonoiden)Achillea millefolium, water-soluble extract (containing 3% flavonoids) 11 Polysorbatpolysorbate 1010 Konservierungsmittelpreservative 11 Kojisäurekojic acid 55 TiO₂TiO₂ 11 Tocopheryllinoleattocopheryl 22 Panthenolpanthenol 11 Phenylbenzimidazol-5-sulfonsäurePhenylbenzimidazole-5-sulfonic acid 66 Triethanolamintriethanolamine 3,13.1 Wasser, adWater, ad 100100

Beispiel 17: GelExample 17: Gel Bestandteileingredients %% Ascorbylpalmitatascorbyl 33 Sohakuhl (Maulbeeren) wasserlöslicher ExtraktSohakuhl (Mulberries) water-soluble extract 2020 Tocopheryllinoleattocopheryl 0,50.5 Polysorbatpolysorbate 66 CarbopolCarbopol 11 Triethanolamintriethanolamine 1,61.6 Konservierungsmittelpreservative 11 Kojisäurekojic acid 0,10.1 Phenylbenzimidazol-5-sulfonsäurePhenylbenzimidazole-5-sulfonic acid 0,10.1 TiO₂TiO₂ 11 Panthenolpanthenol 11 Wasser, adWater, ad 100100

Beispiel 18: GelExample 18: Gel Bestandteileingredients %% Ascorbylpalmitatascorbyl 0,50.5 Sohakuhl (Maulbeeren) wasserlöslicher ExtraktSohakuhl (Mulberries) water-soluble extract 11 Polysorbatpolysorbate 66 CarbopolCarbopol 11 Triethanolamintriethanolamine 4,24.2 Konservierungsmittelpreservative 11 Kojisäurekojic acid 55 TiO₂TiO₂ 1010 Tocopheryllinoleattocopheryl 11 Panthenolpanthenol 11 Phenylbenzimidazol-5-sulfonsäurePhenylbenzimidazole-5-sulfonic acid 66 Wasser, adWater, ad 100100

Beispiel 19Example 19 Bestandteileingredients %% Cetylalkoholcetyl alcohol 55 Glycerylstearat SEGlyceryl stearate SE 33 Capryl/Caprylat-triglyceridCaprylic / caprylate triglyceride 33 P E G 6000-DistearatP E G 6000 distearate 11 Achillea millefolium-ExtraktAchillea millefolium extract 11 Lakritzenextraktlicorice extract 0,050.05 AscorbylpalmitätAscorbylpalmität 0,50.5 Tocopheryllinoleattocopheryl 0,20.2 TitandioxidTitanium dioxide 22 Glykolsäureglycolic acid 55 Konservierungsmittelpreservative 9,59.5 Xanthangummixanthan gum 0,30.3 NH₄OH, adNH₄OH, ad pH 4pH 4 H₂O, dest., adH₂O, dist., Ad 100100

Beispiel 20Example 20 Bestandteileingredients %% Achillea millefolium-ExtraktAchillea millefolium extract 22 Kojisäurekojic acid 0,50.5 Ascorbylpalmitatascorbyl 0,20.2 α-Hydroxysäure als Glykolsäureα-hydroxy acid as glycolic acid 55 Lotiongrundlage, adLotion foundation, ad 100100

In den folgenden Beispielen wurde als Lakritzenextrakt der von der Firma Nikko Chemicals, Japan, hergestellte Lakritzenextrakt TP (Glycyrrhiza Glabra) verwendet. Die Prozentangaben beziehen sich auf das Gewicht.In the following examples the licorice extract was the Licorice extract produced by Nikko Chemicals, Japan TP (Glycyrrhiza Glabra). The percentages refer to the weight.

Beispiel 21Example 21 Bestandteileingredients %% Lakritzenextraktlicorice extract 0,050.05 Extrakt von Achillea millefoliumExtract of Achillea millefolium 3,03.0 Ascorbylpalmitatascorbyl 0,50.5 Cremegrundlage, adCream base, ad 100100

Beispiel 22Example 22 Bestandteileingredients %% Lakritzenextraktlicorice extract 0,10.1 Ascorbylpalmitatascorbyl 1,01.0 Tocopheryllinoleattocopheryl 0,50.5 Lotiongrundlage, adLotion foundation, ad 100100

Beispiel 23Example 23 Bestandteileingredients %% Lakritzenextraktlicorice extract 4,04.0 Achillea millefolium-ExtraktAchillea millefolium extract 3,03.0 Tocopheryllinoleattocopheryl 0,50.5 Butylmethoxydibenzoylmethanbutylmethoxydibenzoylmethane 1,51.5 TitandioxidTitanium dioxide 5,05.0 Kamillenextraktchamomile extract 0,10.1 I P MI P M 2,02.0 BHTBHT 0,040.04 Konservierungsmittelpreservative 0,50.5 Stearinsäurestearic acid 2,02.0 Na-EDTANa-EDTA 0,10.1 DEA-CetylphosphatDEA cetyl phosphate 3,53.5 Cetylalkoholcetyl alcohol 0,20.2 Glycerinstearatglyceryl stearate 2,02.0 destilliertes Wasser, addistilled water, ad 100100

Die erfindungsgemäßen Zusammensetzungen wurden nach Durch­ führung von umfangreichen Untersuchungen aufgefunden. Als Bewertungskriterien wurden die willkürlichen Bewertungszif­ fern 0, 1, 2 und 3 zur Beurteilung der Fleckenanzahl, der Fleckenfarbe und der Kontraststärke verwendet. Die Hauttypen wurden je nach Neigung zu Sonnenbrand bzw. Bräunung in vier Kategorien eingeteilt. Die Untersuchungen wurden an weibli­ chen und männlichen freiwilligen Versuchspersonen durchge­ führt. Das Alter der Versuchspersonen lag zwischen 50 und 92 Jahren. Es wurden nur solche Versuchspersonen herangezogen, die an beiden Handrücken symmetrische Altersflecken aufwie­ sen, wobei eine angemessene Anzahl an derartigen Flecken ausreichend dunkel gefärbt und kontrastreich war.The compositions of the invention were after leadership of extensive investigations. When Evaluation criteria were the arbitrary rating 0, 1, 2 and 3 for assessing the number of stains, the Spot color and contrast strength used. The skin types were sunburned or suntanned into four, depending on your preference Categories divided. The investigations were female male and male volunteers leads. The age of the subjects was between 50 and 92 Years. Only such subjects were used the on both backs symmetrical age spots aufwie with a reasonable number of such spots was sufficiently dark colored and rich in contrast.

Die Untersuchungen wurden jeweils mit den Hauptbestandteilen allein und anschließend mit verschiedenen Kombinationen in unterschiedlichen Dosierungen (Konzentrationen) durchge­ führt.The investigations were each with the main components alone and then with different combinations in different dosages (concentrations) durchge leads.

Ascorbinsäure und ihre Derivate zeigten eine bestimmte Wir­ kung, jedoch nur bei relativ hohen Dosen. Auch die vorer­ wähnten Flavonoide wurden allein getestet. Auch sie zeigten eine bestimmte Wirkung.Ascorbic acid and its derivatives showed a particular we kung, but only at relatively high doses. Also the vorer mentioned flavonoids were tested alone. They too showed a certain effect.

Es wurde überraschenderweise festgestellt, daß eine Kombina­ tion dieser beiden Bestandteile eine ausgeprägte Wirkungs­ steigerung hervorrief, selbst wenn man die Einzelbestand­ teile in geringeren Dosen einsetzte. Die Zugabe von Toco­ pherylderivaten oder von Kojisäure verstärkte zusätzlich die Aufhellungswirkung. Die einzelnen Kombinationen zeigten je­ weils eine synergistische Wirkung.It was surprisingly found that a Kombina tion of these two components a pronounced effect increase, even if the individual stock used parts in lower doses. The addition of Toco pheryl derivatives or kojic acid additionally enhanced Whitening effect. The individual combinations ever showed because a synergistic effect.

Es ist wahrscheinlich, daß die verschiedenen Bestandteile und insbesondere Ascorbinsäure und deren Derivate sowie die Flavonoide ihren Einfluß auf verschiedenen Wegen ausüben. It is likely that the different ingredients and in particular ascorbic acid and its derivatives and the Flavonoids exert their influence in different ways.  

Dies gilt auch für Kojisäure, die offensichtlich ein Enzym, das die Melaninbildung verstärkt, inaktiviert.This also applies to kojic acid, which is obviously an enzyme which enhances melanin formation, inactivates.

Die Aufhellungswirkung der erfindungsgemäßen Zusammensetzun­ gen ist sehr ausgeprägt. Eine Anwendungsdauer von etwa 2 bis 3 Monaten ist ausreichend.The whitening effect of the composition according to the invention is very pronounced. An application period of about 2 to 3 months is sufficient.

Wie vorstehend erwähnt, zeigen offensichtlich Ascorbinsäure und deren Derivate bei gleichzeitiger Verwendung mit den an­ gegebenen Flavonoiden eine synergistische Wirkung, die durch Bestandteile, wie Tocopherol oder Kojisäure, noch weiter verstärkt wird.As mentioned above, ascorbic acid apparently and their derivatives when used with the given flavonoids have a synergistic effect by Ingredients, such as tocopherol or kojic acid, even further is reinforced.

Claims (12)

1. Topisch anzuwendendes Mittel zur Aufhellung von Haut- und Hautflecken in Form von Lösungen, Lotionen, Gels, Sprühmitteln oder Cremes, enthaltend eine Kombination aus einer wirksamen Menge eines Flavonoids und einer wirksamen Menge eines DOPA-Chinon-Reduktionsmittels, gegebenenfalls in Kombination mit einem Sonnen­ schutzmittel, einem Mittel zur Unterdrückung der Tyrosi­ nase-Aktivität und/oder einem Tocopherylderivat.1. Topically applied skin lightening agent and skin spots in the form of solutions, lotions, gels, Sprays or creams containing a combination from an effective amount of a flavonoid and a effective amount of a DOPA quinone reducing agent, optionally in combination with a sun a means of suppressing tyrosis nase activity and / or a tocopheryl derivative. 2. Mittel nach Anspruch 1, dadurch gekennzeichnet, daß das Flavonoid in Form eines Pflanzenextrakts oder in Form eines gereinigten Präparats aus Achillea Millefolium, Calendula, Salbei, Zaubernuß und Maulbeeren vorliegt.2. Composition according to claim 1, characterized in that the Flavonoid in the form of a plant extract or in the form a purified preparation from Achillea Millefolium, Calendula, sage, witch hazel and mulberry present. 3. Mittel nach Anspruch 1 oder 2, dadurch gekennzeichnet, daß es sich beim Sonnenschutzmittel um ein Mittel zum Schutz gegen UVA-, UVB, IR- und/oder sichtbares Licht, wie Octylmethoxycinnamat, Butylmethoxydibenzoylmethan und Titandioxid, handelt.3. Composition according to claim 1 or 2, characterized that the sunscreen is a means to Protection against UVA, UVB, IR and / or visible light, such as octylmethoxycinnamate, butylmethoxydibenzoylmethane and titanium dioxide. 4. Mittel nach einem der Ansprüche 1 bis 3, dadurch gekenn­ zeichnet, daß als DOPA-Chinon-Reduktionsmittel Ascorbin­ säure, Ascorbylpalmitat, Ascorbylstearat, Magnesiumas­ corbylphosphat oder ein beliebiges anderes geeignetes physiologisch verträgliches Derivat von Ascorbinsäure vorliegt.4. Composition according to one of claims 1 to 3, characterized marked records that as DOPA quinone reducing agent ascorbin acid, ascorbyl palmitate, ascorbyl stearate, magnesium corbyl phosphate or any other suitable Physiologically acceptable derivative of ascorbic acid is present. 5. Mittel nach einem der Ansprüche 1 bis 4, dadurch gekenn­ zeichnet, daß es ein Tocopherylderivat enthält.5. Composition according to one of claims 1 to 4, characterized marked records that it contains a tocopheryl derivative. 6. Mittel nach einem der Ansprüche 1 bis 5, dadurch gekenn­ zeichnet, daß es Kojisäure enthält. 6. Composition according to one of claims 1 to 5, characterized marked records that it contains kojic acid.   7. Mittel nach einem der Ansprüche 1 bis 6, dadurch gekenn­ zeichnet, daß es etwa 0,1 bis etwa 30 Gew.-% gereinigtes Flavonoid oder ein Pflanzenextrakt mit einer äquivalen­ ten Menge an Flavonoid enthält.7. Composition according to one of claims 1 to 6, characterized gekenn characterized in that it is from about 0.1 to about 30% by weight of purified Flavonoid or a plant extract with an equivalency th amount of flavonoid contains. 8. Mittel nach einem der Ansprüche 1 bis 7, dadurch gekenn­ zeichnet, daß es etwa 0,1 bis etwa 5 Gew.-% an Ascorbin­ säure oder einem Derivat davon enthält.8. Composition according to one of claims 1 to 7, characterized marked indicates that there are about 0.1 to about 5% by weight of ascorbic acid acid or a derivative thereof. 9. Mittel nach einem der Ansprüche 1 bis 8, dadurch gekenn­ zeichnet, daß es etwa 1 bis 10 Gew.-% eines Sonnen­ schutzmittels enthält.9. Composition according to one of claims 1 to 8, characterized marked records that it is about 1 to 10 wt .-% of a sun contains protective agent. 10. Mittel nach einem der Ansprüche 1 bis 9, dadurch gekenn­ zeichnet, daß es etwa 0,1 bis etwa 5 Gew.-% Kojisäure enthält.10. Composition according to one of claims 1 to 9, characterized marked that it contains about 0.1 to about 5% by weight kojic acid contains. 11. Kosmetisches Hautaufhellungsmittel zur topischen Anwen­ dung, enthaltend Ascorbinsäure oder ein Derivat davon und ein Flavonoid, gegebenenfalls zusammen mit anderen Bestandteilen, Verdünnungsmitteln, Cremegrundlagen und/oder Gelbildungsmitteln.11. Cosmetic skin lightening agent for topical application containing ascorbic acid or a derivative thereof and a flavonoid, optionally together with others Ingredients, diluents, cream bases and / or gelling agents. 12. Mittel nach Anspruch 2, dadurch gekennzeichnet, daß der Pflanzenextrakt ein Lakritzenextrakt (Glycyrrhiza Glabra) ist.12. Composition according to claim 2, characterized in that the Plant extract a licorice extract (Glycyrrhiza Glabra) is.
DE4227806A 1991-08-23 1992-08-21 Topical compsn. for lightening skin or skin spots - contg. flavonoid, reducing agent for dopa-quinone and opt. sun protectant, suppressant for tyrosinase activity and tocopherol deriv. Withdrawn DE4227806A1 (en)

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CA2076467A1 (en) 1993-02-24
ES2050074B1 (en) 1994-12-16
GB2259014A (en) 1993-03-03
AU654030B2 (en) 1994-10-20
GB2259014B (en) 1996-02-28
ES2050074A1 (en) 1994-05-01
IL99291A (en) 1997-04-15
PT100800A (en) 1994-02-28
FR2680466A1 (en) 1993-02-26
CH684739A5 (en) 1994-12-15
FR2680466B3 (en) 1993-11-19
PT100800B (en) 1999-07-30
AU2122092A (en) 1993-02-25
GB9217821D0 (en) 1992-10-07
IL99291A0 (en) 1992-07-15

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